• Title/Summary/Keyword: transdermal delivery

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Effect of Enhancers and Pressure Sensitive Adhesives on the Transdermal Delivery of Fentanyl

  • Lee, Ji-Young;Jang, Joon-Ho;Choi, Hoo-Kyun
    • Journal of Pharmaceutical Investigation
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    • v.38 no.4
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    • pp.223-228
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    • 2008
  • The purpose of this study was to investigate the feasibility of developing transdermal drug delivery system (TDDS) for fentanyl used for the management of chronic cancer pain. The effect of type of pressure sensitive adhesive on the permeation of fentanyl from polyisobutylene (PIB), silicone and acrylic adhesive was evaluated. Due to the good adhesive force and relatively steady flux for 3 days, both acrylic and PIB adhesives were chosen for further study. The permeation rate of fentanyl was the highest from acrylic adhesive with hydroxyl functional group. Permeation rate increased linearly as the concentration of fentanyl in acrylic adhesive was increased from 2.5% to 10%. In case of PIB adhesive, crystals of fentanyl were developed above 5% drug load. $Crovol^{(R)}$ A40, $Crovol^{(R)}$ PK40 and Plurol $oleique^{(R)}$ provided higher flux of fentanyl.

Design of Transdermal Delivery System Using New Film-Forming Agents (신규 필름형성제를 이용한 경피흡수제제의 설계)

  • Choi, Yang-Gyu;Kim, Young-So;Kim, Jung-Ju;Sim, Young-Chul
    • Journal of Pharmaceutical Investigation
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    • v.33 no.3
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    • pp.163-169
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    • 2003
  • In order to develop a film-forming transdermal drug delivery system, polyurethane (PU) based on poly(ethylene glycol) and poly(tetramethylene oxide) was synthesized and characterized. The synthesized PU was blended with Gantrez ES 225 (GT) to improve the adhesion property of film-forming agent to the skin. When film-forming gel formulation containing 3% ketoprofen (KP) was applied, transparent thin film was obtained within 5 minutes and adhered to the skin for 8 hours. In vitro percutaneous absortion studies were performed to determine the rate of ketoprofen absorption through guinea pig skin. A prominent effect of limonene on the skin permeability of ketoprofen was observed among the various skin permeation enhancers investigated. Considering mechanica properties of film and skin permeability of ketoprofen, 2% of limonene was optimal content in the film forming transdermal formulation.

Transdermal Delivery of Diclofenac Using Microemulsions

  • Kweon, Jang-Hoon;Chi, Sang-Cheol;Park, Eun-Seok
    • Archives of Pharmacal Research
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    • v.27 no.3
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    • pp.351-356
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    • 2004
  • A transdermal preparation containing diclofenac diethylammonium (DDA) was developed using an O/W microemulsion system. Of the oils tested, lauryl alcohol was chosen as the oil phase of the microemulsion, as it showed a good solubilizing capacity and excellent skin permeation rate of the drug. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and cosurfactant for microemulsion formation, and the effect of these additives on skin permeation of DDA was evaluated with excised rat skins. The optimum formulation of the microemulsion consisted of 1.16% of DDA, 5% of lauryl alcohol, 60% of water in combination with the 34.54% of Labrasol (surfactant)/ethanol (cosurfactant) (1:2). The efficiency of formulation in the percutaneous absorption of DDA was dependent upon the contents of water and lauryl alcohol as well as Labrasol: ethanol mixing ratio. It was concluded that the percutaneous absorption of DDA from microemulsions was enhanced with increasing the lauryl alcohol and water contents, and with decreasing the Labrasol:ethanol mixing ratio in the formulation.

Establishment Percutaneous Administration Method in Beagle Dog

  • Han, Su-Cheol;Bae, Ju-Hyun;Cha, Shin-Woo;Jiang, Cheng-Zhe;Tarumoto Y.;Kim, Choong-Yong;Chung, Moon-Koo
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2003.10b
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    • pp.154-154
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    • 2003
  • The primary routes of drug administration include oral, intramuscular, subcutaneous and intravenous dosing for toxicological risk assessment purpose in dog. There has been an increase applying transdermal patches as an alternate method for systemic delivery. The present study was performed to establish the transdermal delivery method of medicated ointment, liquid and powder material to beagle dog.(omitted)

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Development of Automated Diffusion Cell for Determining In Vitro Drug Release from Transdermal Device (경피흡수제형의 in vitro 약물방출실험을 위한 연속확산 장치의 개발)

  • Byun, Young-Rho;Choi, Young-Kweon;Jeong, Seo-Young;Kim, Young-Ha
    • YAKHAK HOEJI
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    • v.34 no.3
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    • pp.161-165
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    • 1990
  • An automated, simple, and reliable method was developed for determining in vitro drug release rate from transdermal delivery dosage forms. The patch is held in position in the heating block by sandwiching it between the middle plate and the bottom plate of diffusion cell. The dissolution profile of the commercially available transdermal scopolamine patch was determined over a 72-h period, and the results were compared with those obtained with other methods; paddle-over-disk method, reciprocating method, and diffusion cell method. It was demonstrated that the flow-through method is equivalent in terms of release rate profile and accumulated released drug amount over the lifetime of the dosage form tested. Also this method is simple, reliable and reproducible. Therefore, this technique can be used in a quality control for assuring product uniformity.

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Preparation and Evaluation of Aceclofenac Microemulsion for Transdermal Delivery System

  • Yang, Jae-Heon;Kim, Young-Il;Kim, Kyung-Mi
    • Archives of Pharmacal Research
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    • v.25 no.4
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    • pp.534-540
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    • 2002
  • To develop novel transdermal formulation for aceclofenac, microemulsion was prepared for increasing its skin permeability. Based on solubiity and phase studies, oil and surfactant was selected and composition was determined. Microemulsion was spontaneously prepared by mixing ingredients and the physicochemical properties such was investigated. The mean diameters of microemulsion were approximately 90 nm and the system was physically stable at room temperature at least for 3 months. In addition, the in vitro and in vivo performance of microemulsion formulation was evaluated. Aceclofenac was released from microemulsion in acidic aqueous medium, and dissolved amounts of aceclofenac was approximately 30% after 240 min. Skin permeation of aceclofenac from microemulsion formulation was higher than that of cream. Following transdermal application of aceclofenac preparation to delayed onset muscle soreness, serum creatine phosphokinase and lactate dehydrogenase activity was significantly reduced by aceclofenac. Aceclofenac in microemulsion was more potent than cream in the alleviation of muscle pain. Therefore, the microemulsion formulation of aceclofenac appear to be a reasonable transdermal delivery system of the drug with enhanced skin permeability and efficacy for the treatment of muscle damage.

Development of Transdermal Drug Delivery System for the Combination of Physostigmine and Procyclidine

  • Park, Soon-Cheol;Choi, Hoo-Kyun
    • Journal of Pharmaceutical Investigation
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    • v.31 no.3
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    • pp.181-184
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    • 2001
  • The purpose of this study was to develop transdermal drug delivery system (TDDS) for the combination of physostigmine and procyclidine. The effects of various pressure sensitive adhesives (PSA) on the percutaneous absorption of procyclidine across hairless mouse skin were evaluated to select an appropriate PSA. In addition, the influences of various vehicles on the percutaneous absorption of procyclidine from PSA matrix across hairless mouse skin were evaluated using flow-through diffusion cell system at $37^{\circ}C$. Physostigmine did not have any influence on the permeation rate of procyclidine. The flux of procyclidine was the highest in silicone and PIB and was relatively lower in SIS, Acryl, and SBS adhesive matrices, however, their use was limited by the crystallization of the drug in the matrix. Among acrylic adhesives, the permeability of procyclidine was the highest from poly (ethylene oxide) grafted acrylic adhesive. Some enhancers show different enhancing effect depending on the drug, however, many of the tested enhancers showed enhancing effect for the permeation of both procyclidine and physostigmine to some extent. $Crovol^{\circledR}$ EP 40 showed the highest enhancing effect on the permeation of both compounds. The size of TDDS to provide required permeation rate was estimated to be $35\;cm^2$ based on available information.

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Transdermal Delivery of Porcine Placenta Extracts using Linolenic Acid-based Emulsion Formulations

  • Kim, Dong-Chan;Noh, Sang-Myoung;Park, Ki-Tae;Kim, Young-Bong;Baek, Kwang-Hyun;Oh, Yu-Kyoung
    • Journal of Pharmaceutical Investigation
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    • v.37 no.5
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    • pp.281-286
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    • 2007
  • For transdermal delivery of porcine placenta extract (PPE), various emulsion formulations were prepared and evaluated. Polysorbate surfactants were used as emulsifiers and various C-18 unsaturated fatty acids as enhancers. The skin permeation of PPE was tested using a cellulose nitrate membrane-loaded Franz cell apparatus. Among emulsifiers, Tween 20 provided higher penetration effect than did Tween 80. Meanwhile, of various fatty acids, linolenic acid (18:3) revealed the highest skin permeation of PPE than the other C-18 unsaturated fatty acids. Stability of PPE emulsions was determined by cycles of freezing and thawing processes. The stability of emulsions depended on the percentage of Tween 20. Minimum 20% of Tween 20 was required to stabilize emulsions at room temperature for several days. Taken together, our results suggest that Tween 20 and linolenic acids might be key components to formulate PPE emulsion to provide the desirable skin permeability and stability.

Calcitonin Transport through Skin Using Iontophoresis

  • Kim, Kyung-Min;Oh, Seaung-Youl
    • Journal of Pharmaceutical Investigation
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    • v.41 no.1
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    • pp.9-17
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    • 2011
  • The objective of this work is to study transdermal delivery of calcitonin using iontophoresis and to evaluate various factors which affect the transdermal transport. We have studied the effect of polarity, current density, drug concentration, penetration enhancers (isopropyl myristate [IPM] and ethanol) and laser treatment on transdermal flux and the results were compared. We also investigated the iontophoretic flux from microemulsions containing calcitonin together with oleic acid (OA) or IPM. In vitro flux study was performed at $33^{\circ}C$, using side-by-side diffusion cell and full thickness hairless mouse skin. Anodal delivery at pH 3.0 was much larger than cathodal and passive delivery, due to the positive charge of calcitonin. Cumulative amount delivered (CUM) by cathodal or passive delivery was close to zero for 10 hours. The pretreatment of skin by neat IPM markedly increased the CUM anodically. CUM increased as the current density, drug concentration or the duration of IPM treatment increased. Microemulsion containing IPM or oleic acid was prepared and the phase diagram was constructed. CUM also increased when IPM was incorporated into a microemulsion. OA microemulsion showed similar enhancing effect to IPM microemulsion. The delivery of calcitonin from 70% (v/v) ethanol aqueous solution showed a large increase in flux. Laser treatment of skin before flux experiment exhibited about 2 fold increase in total calcitonin amount transported for 12 hours, when compared to that delivered by IPM microemulsion. Based on these results, we have evaluated the possibility of delivering enough amount of calcitonin to reach the therapeutic level. The data suggest that it is highly possible to deliver clinically effective amount of calcitonin using iontophoresis patch with small area (<10 $cm^2$).

Transdermal Delivery of FITC-Ovalbumin with Microneedle System (마이크로 피부침을 이용한 FITC-OVA의 경피흡수)

  • Jang, Woo-Young;Lee, Chang-Rae;Seo, Seong-Mi;Lee, Bong;Kim, Moon-Suk;Khang, Gil-Son;Lee, Han-Gu;Lee, Hai-Bang
    • Journal of Pharmaceutical Investigation
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    • v.35 no.6
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    • pp.403-409
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    • 2005
  • For transdermal delivery of large molecular drugs such as vaccine and protein drugs, novel microneedle treatment device with roll was designed. The roll dimension is 1.43 cm diameter and 2.8 cm perimeter. Total number of microneedle on the roll is 3,360 with $230\;{\mu}m$ height and $740\;{\mu}m$ distance. The pore with $150\;{\mu}m$ depth and $35\;{\mu}m$ diameter on the skin was made by the designed microneedle device. This system could be achieved without pain. The permeation rates of FITC labelled ovalbumin (FITC-OVA, molecular weight: 45,000 g/mol) as a model protein were determined by modified Franz diffusion cells using skins of hairless mice or SD rats which were treated by using microneedle device two or four times. The average penetration fluxes of model protein increased from 674 to $872\;{\mu}g/cm^{2}{\cdot}hr$ as the number of treatment to make pore increased from two to four times. In conclusion, we confirmed the possibility of using the designed microneedle treatment device for transdermal delivery of the large molecular drugs.